| Bioactivity | CDK/HDAC-IN-3 is an orally active HDACs/CDKs dual inhibitor. CDK/HDAC-IN-3 has potent and selective inhibition of CDK9, CDK12, CDK13, HDAC1, HDAC2 and HDAC3 with IC50 values of 98.32 nM, 98.85 nM, 100 nM, 62.12 nM, 93.28nM and 82.87 nM. CDK/HDAC-IN-3 can be used for the acute myeloid leukemia (AML) [1]. |
| Target | IC50: 98.32 nM (CDK9), 98.85 nM (CDK12), 100 nM (CDK13), 62.12 nM (HDAC1), 93.28nM (HDAC2) and 82.87 nM (HDAC3), 0.72 μM (U937 cell), 1.43μM (HL-60 cell), 1.63μM (SKNO-1 cell) and 0.89 μM (Kaumi-1 cell). |
| Invitro | CDK/HDAC-IN-3 (compound 33a) (1μM) 对 CDK9、CDK12、CDK13、HDAC1、HDAC2 和 HDAC3 具有有效和选择性的抑制作用，IC50 值为 98.32 nM、98.85 nM、100 分别为 nM、62.12 nM、93.28 nM 和 82.87 nM[1]。CDK/HDAC-IN-3 (0.5 μM, 1.0 μM) 显著诱导白血病干细胞样细胞分化并抑制 AML 增殖[1]。CDK/HDAC-IN-3 (0.5 μM, 1.0 μM, 2.0 μM) 显着诱导 LSCs 分化[1]。CDK/HDAC-IN-3 对 U937、HL-60、SKNO-1 和 Kaumi-1 细胞具有抑制作用，IC50 值分别为 0.72 μM、1.43μM、1.63μM 和 0.89 μM [1]。 Cell Proliferation Assay[1] Cell Line: |
| In Vivo | CDK/HDAC-IN-3 (compound 33a) (i.v., p.o.; 5, 25 mg/kg) 具有良好的口服生物利用度[1]。 Animal Model: |
| Name | CDK/HDAC-IN-3 |
| Formula | C24H18Cl2N6O3 |
| Molar Mass | 509.34 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Liu Y, et al. Discovery of novel and bioavailable histone deacetylases and cyclin-dependent kinases dual inhibitor to impair the stemness of leukemia cells. Eur J Med Chem. 2023;249:115140. |